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A comparison of some of the pharmacological properties of etintidine, a new histamine H2-receptor antagonist, with those of cimetidine, ranitidine and tiotidine.
J Pharmacol Exp Ther. 1983 Jan; 224(1):171-9.JP

Abstract

Etintidine is a competitive antagonist of histamine H2-receptors in the isolated spontaneously beating guinea-pig right atrium with a pA2 value of 6.6 relative to values of 6.2, 6.7 and 7.3 for cimetidine, ranitidine and tiotidine, respectively. Low affinities for histamine H1 (pA2 = 4.2), cholinergic (pA2 = 4.4) and beta adrenergic (pA2 = 3.8) receptors indicated that etintidine has a high degree of specificity for the H2-receptor. The other antagonists studied also exhibited low affinities for these receptors; however, relative to these compounds, etintidine demonstrated a somewhat greater affinity for cholinergic receptors. Etintidine also antagonized basal gastric acid secretion in the conscious gastric fistula rat and histamine, pentagastrin, carbachol, 2-deoxy-D-glucose and meal-stimulated gastric acid secretion in conscious gastric fistula and Heidenhain pouch dogs. After oral administration to conscious Heidenhain pouch dogs, ED50 values for the inhibition of near maximal gastric acid secretion stimulated by histamine were 7.1, 5.4, 0.74 and 0.69 mumol/kg for cimetidine, etintidine, ranitidine and tiotidine, respectively. Onset and duration of the gastric antisecretory activities of the four compounds were similar. The order of potency as histamine H2-receptor and gastric antisecretory antagonists was cimetidine less than etintidine less than ranitidine less than tiotidine. Based on the high degree of specificity for the H2-receptor and its potent gastric antisecretory activity, etintidine may prove to be a useful agent in the treatment of peptic ulcer disease.

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Publisher Full Text

Authors

Cavanagh RL
No affiliation info available
Usakewicz JJ
No affiliation info available
Buyniski JP
No affiliation info available

MeSH

Adrenergic beta-AntagonistsAnimalsCimetidineDogsFemaleFuransGastric JuiceGuanidinesGuinea PigsHeart RateHistamine H1 AntagonistsHistamine H2 AntagonistsImidazolesIn Vitro TechniquesMaleMyocardial ContractionParasympatholyticsRanitidineRatsRats, Inbred StrainsThiazolesUterine Contraction

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

6129316

Citation

Cavanagh, R L., et al. "A Comparison of some of the Pharmacological Properties of Etintidine, a New Histamine H2-receptor Antagonist, With Those of Cimetidine, Ranitidine and Tiotidine." The Journal of Pharmacology and Experimental Therapeutics, vol. 224, no. 1, 1983, pp. 171-9.
Cavanagh RL, Usakewicz JJ, Buyniski JP. A comparison of some of the pharmacological properties of etintidine, a new histamine H2-receptor antagonist, with those of cimetidine, ranitidine and tiotidine. J Pharmacol Exp Ther. 1983;224(1):171-9.
Cavanagh, R. L., Usakewicz, J. J., & Buyniski, J. P. (1983). A comparison of some of the pharmacological properties of etintidine, a new histamine H2-receptor antagonist, with those of cimetidine, ranitidine and tiotidine. The Journal of Pharmacology and Experimental Therapeutics, 224(1), 171-9.
Cavanagh RL, Usakewicz JJ, Buyniski JP. A Comparison of some of the Pharmacological Properties of Etintidine, a New Histamine H2-receptor Antagonist, With Those of Cimetidine, Ranitidine and Tiotidine. J Pharmacol Exp Ther. 1983;224(1):171-9. PubMed PMID: 6129316.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - A comparison of some of the pharmacological properties of etintidine, a new histamine H2-receptor antagonist, with those of cimetidine, ranitidine and tiotidine. AU - Cavanagh,R L, AU - Usakewicz,J J, AU - Buyniski,J P, PY - 1983/1/1/pubmed PY - 1983/1/1/medline PY - 1983/1/1/entrez SP - 171 EP - 9 JF - The Journal of pharmacology and experimental therapeutics JO - J Pharmacol Exp Ther VL - 224 IS - 1 N2 - Etintidine is a competitive antagonist of histamine H2-receptors in the isolated spontaneously beating guinea-pig right atrium with a pA2 value of 6.6 relative to values of 6.2, 6.7 and 7.3 for cimetidine, ranitidine and tiotidine, respectively. Low affinities for histamine H1 (pA2 = 4.2), cholinergic (pA2 = 4.4) and beta adrenergic (pA2 = 3.8) receptors indicated that etintidine has a high degree of specificity for the H2-receptor. The other antagonists studied also exhibited low affinities for these receptors; however, relative to these compounds, etintidine demonstrated a somewhat greater affinity for cholinergic receptors. Etintidine also antagonized basal gastric acid secretion in the conscious gastric fistula rat and histamine, pentagastrin, carbachol, 2-deoxy-D-glucose and meal-stimulated gastric acid secretion in conscious gastric fistula and Heidenhain pouch dogs. After oral administration to conscious Heidenhain pouch dogs, ED50 values for the inhibition of near maximal gastric acid secretion stimulated by histamine were 7.1, 5.4, 0.74 and 0.69 mumol/kg for cimetidine, etintidine, ranitidine and tiotidine, respectively. Onset and duration of the gastric antisecretory activities of the four compounds were similar. The order of potency as histamine H2-receptor and gastric antisecretory antagonists was cimetidine less than etintidine less than ranitidine less than tiotidine. Based on the high degree of specificity for the H2-receptor and its potent gastric antisecretory activity, etintidine may prove to be a useful agent in the treatment of peptic ulcer disease. SN - 0022-3565 UR - https://www.unboundmedicine.com/medline/citation/6129316/A_comparison_of_some_of_the_pharmacological_properties_of_etintidine_a_new_histamine_H2_receptor_antagonist_with_those_of_cimetidine_ranitidine_and_tiotidine_ L2 - https://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=6129316 DB - PRIME DP - Unbound Medicine ER -